1135021-79-2Relevant articles and documents
Reactions of 4,5-dihydro-1,4-benzothiazepin-3(2H)-one 1,1-dioxide and 1,5-dihydro-4,1-benzothiazepin-2(3H)-one 4,4-dioxide derivatives with vilsmeier reagent and DMFDMA
Tarasiuk, Taras M.,Volovnenko, Tatyana A.,Popov, Kirill S.,Medviediev, Volodymyr V.,Shishkin, Oleg V.,Volovenko, Yulian M.
, p. 755 - 759 (2014)
The regioselectivity of the interaction between isomeric 4,5-dihydro-1,4-benzothiazepin-3(2H)-one 1,1-dioxide and 1,5-dihydro-4,1- benzothiazepin-2(3H)-one 4,4-dioxide derivatives with the Vilsmeier reagent and DMFDMA (N,N-dimethylformamide dimethylacetal
META-DIAMIDE COMPOUNDS FOR CONTROLLING INVERTEBRATE PESTS
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Page/Page column 46, (2020/06/19)
Disclosed are compounds of Formula (1), N-oxides, and salts thereof, wherein Q, X, Y, A1, A2, L, R1, R2, R3, R4, R5, R6a, R6b, R7 and R8 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (1) and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the disclosure.
N-Benzyl-4-((heteroaryl)methyl)benzamides: A New Class of Direct NADH-Dependent 2-trans Enoyl-Acyl Carrier Protein Reductase (InhA) Inhibitors with Antitubercular Activity
Guardia, Ana,Gulten, Gulcin,Fernandez, Raquel,Gómez, Jesus,Wang, Feng,Convery, Maire,Blanco, Delia,Martínez, María,Pérez-Herrán, Esther,Alonso, Marta,Ortega, Fátima,Rullás, Joaquín,Calvo, David,Mata, Lydia,Young, Robert,Sacchettini, James C.,Mendoza-Losana, Alfonso,Remui?án, Modesto,Ballellpages, Lluís,Castro-Pichel, Julia
, p. 687 - 701 (2016/04/20)
Isoniazid (INH) remains one of the cornerstones of antitubercular chemotherapy for drug-sensitive strains of M.tuberculosis bacteria. However, the increasing prevalence of multidrug-resistant (MDR) and extensively drug-resistant (XDR) strains containing mutations in the KatG enzyme, which is responsible for the activation of INH into its antitubercular form, have rendered this drug of little or no use in many cases of drug-resistant tuberculosis. Presented herein is a novel family of antitubercular direct NADH-dependent 2-trans enoyl-acyl carrier protein reductase (InhA) inhibitors based on an N-benzyl-4-((heteroaryl)methyl)benzamide template; unlike INH, these do not require prior activation by KatG. Given their direct InhA target engagement, these compounds should be able to circumvent KatG-related resistance in the clinic. The lead molecules were shown to be potent inhibitors of InhA and showed activity against M.tuberculosis bacteria. This new family of inhibitors was found to be chemically tractable, as exemplified by the facile synthesis of analogues and the establishment of structure-activity relationships. Furthermore, a co-crystal structure of the initial hit with the enzyme is disclosed, providing valuable information toward the design of new InhA inhibitors for the treatment of MDR/XDR tuberculosis.